850664-21-0 Usage
Description
GSK269962A is a selective Rho-associated kinase (ROCK) inhibitor, specifically targeting ROCK1 and ROCK2, which are key regulators of cytoskeletal stability and various cellular functions such as cell adhesion, proliferation, smooth muscle contraction, and stem cell renewal. It exhibits high selectivity for ROCK against a panel of serine/threonine kinases and has demonstrated the ability to block inflammatory cytokine generation and induce vasorelaxation.
Used in Pharmaceutical Industry:
GSK269962A is used as a potent and selective Rho kinase (ROCK) inhibitor for the development of therapeutic agents targeting various diseases and conditions. Its ability to regulate cytoskeletal stability and cellular functions makes it a promising candidate for the treatment of conditions involving abnormal cell adhesion, proliferation, and muscle contraction.
Used in Inflammatory Disease Treatment:
GSK269962A is used as an anti-inflammatory agent for the treatment of inflammatory diseases. Its capacity to block the generation of inflammatory cytokines in lipopolysaccharide-stimulated monocytes suggests its potential in managing inflammatory responses and associated pathological conditions.
Used in Cardiovascular Disease Management:
GSK269962A is used as a vasorelaxation agent for the management of cardiovascular diseases. Its ability to induce vasorelaxation in preconstricted rat aorta indicates its potential in treating conditions related to blood vessel constriction and hypertension.
Used in Hypertension Treatment:
GSK269962A is used as an antihypertensive agent for the treatment of hypertension. Oral administration of GSK269962A at doses of 1-30 mg/kg has been shown to dose-dependently lower blood pressure in spontaneously hypertensive rats, highlighting its potential in managing high blood pressure and related complications.
Check Digit Verification of cas no
The CAS Registry Mumber 850664-21-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,5,0,6,6 and 4 respectively; the second part has 2 digits, 2 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 850664-21:
(8*8)+(7*5)+(6*0)+(5*6)+(4*6)+(3*4)+(2*2)+(1*1)=170
170 % 10 = 0
So 850664-21-0 is a valid CAS Registry Number.
850664-21-0Relevant articles and documents
Discovery of aminofurazan-azabenzimidazoles as inhibitors of rho-kinase with high kinase selectivity and antihypertensive activity
Stavenger, Robert A.,Cui, Haifeng,Dowdell, Sarah E.,Franz, Robert G.,Gaitanopoulos, Dimitri E.,Goodman, Krista B.,Hilfiker, Mark A.,Ivy, Robert L.,Leber, Jack D.,Marino Jr., Joseph P.,Oh, Hye-Ja,Viet, Andrew Q.,Xu, Weiwei,Ye, Guosen,Zhang, Daohua,Zhao, Yongdong,Jolivette, Larry J.,Head, Martha S.,Semus, Simon F.,Elkins, Patricia A.,Kirkpatrick, Robert B.,Dul, Edward,Khandekar, Sanjay S.,Yi, Tracey,Jung, David K.,Wright, Lois L.,Smith, Gary K.,Behm, David J.,Doe, Christopher P.,Bentley, Ross,Chen, Zunxuan X.,Hu, Erding,Lee, Dennis
, p. 2 - 5 (2007/10/03)
The discovery, proposed binding mode, and optimization of a novel class of Rho-kinase inhibitors are presented. Appropriate substitution on the 6-position of the azabenzimidazole core provided subnanomolar enzyme potency in vitro while dramatically improving selectivity over a panel of other kinases. Pharmacokinetic data was obtained for the most potent and selective examples and one (6n) has been shown to lower blood pressure in a rat model of hypertension. Despite many available treatments, hypertension remains a prevalent problem. In fact, some 30% of hypertensive patients are unable to reach their blood pressure goals. Thus, a new anti-hypertensive treatment, which acts on a broader patient population, would be an important addition to existing treatments. A number of vasoconstrictive agents, including angiotensin II, endothelin-1, and urotensin-II, exert their effect through RhoA and the downstream kinase Rho-kinase (ROCK1).1 Because of its central role in the control of smooth muscle contraction, inhibition of ROCK1 could lead to a more broadly efficacious anti-hypertensive agent.2 ROCK1 inhibitors have been shown to relax vascular smooth muscle and lower blood pressure in several animal models of hypertension.3 Therefore, we began an effort to identify potent ROCK1 inhibitors with pharmacokinetic profiles consistent with once daily oral dosing.
